HUP0103212A2 - 2-oxo-2h-quinoline derivatives, pharmaceutical compositions containing them and processes for their preparation - Google Patents
2-oxo-2h-quinoline derivatives, pharmaceutical compositions containing them and processes for their preparationInfo
- Publication number
- HUP0103212A2 HUP0103212A2 HU0103212A HUP0103212A HUP0103212A2 HU P0103212 A2 HUP0103212 A2 HU P0103212A2 HU 0103212 A HU0103212 A HU 0103212A HU P0103212 A HUP0103212 A HU P0103212A HU P0103212 A2 HUP0103212 A2 HU P0103212A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- nha
- general formula
- formula
- oxo
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- LISFMEBWQUVKPJ-UHFFFAOYSA-N quinolin-2-ol Chemical class C1=CC=C2NC(=O)C=CC2=C1 LISFMEBWQUVKPJ-UHFFFAOYSA-N 0.000 title 1
- -1 COOA Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 3
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 abstract 2
- 108010074860 Factor Xa Proteins 0.000 abstract 1
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical group [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 abstract 1
- 229910006074 SO2NH2 Inorganic materials 0.000 abstract 1
- 208000001435 Thromboembolism Diseases 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 235000010290 biphenyl Nutrition 0.000 abstract 1
- 239000004305 biphenyl Substances 0.000 abstract 1
- 125000003739 carbamimidoyl group Chemical group C(N)(=N)* 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 125000006239 protecting group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000000565 sulfonamide group Chemical group 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/20—Oxygen atoms
- C07D215/22—Oxygen atoms attached in position 2 or 4
- C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D215/50—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
- C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Quinoline Compounds (AREA)
Abstract
Az (I) általános képletű új vegyületek - a képletben R és R1 jelentéseegymástól függetlenül H, A, -(CH2)m-R4, -(CH2)m- OA vagy -(CH2)m-Ar,R2 jelentése Ar, (a) vagy (b) általános képletű csoport, R3 jelentéseAr, R4 jelentése CN, COOH, COOA, CONH2, CONHA, CONA2, vagy C(=NH)-NH2,R5 jelentése -C(=NH)-NH2, -NH-C(=NH)-NH2 vagy -C(=O)-N= C(NH2)2,amelyek szubsztituálatlanok vagy -COA, -COOA, -OH csoporttal vagyszokásos amino-védőcsoporttal vannak monoszubsztituálva, vagy (c) vagy(d) képletű csoport, R6 jelentése H, A vagy NH2, Ar jelentése fend-,naftil- vagy bifenilcsoport, amelyek szubsztituálatlanok, vagy A, 3-6szénatomos cikloalkil-, OH, OA, Hal, CN, NO2, CF3, NH2, NHA, NA2,pirrolidin-1-il-, piperidin-1-il-, benziloxi-, SO2NH2, SO2NHA, SO2NA2,-(CH2)n-NH2, -(CH2)n -NHA, -(CH2)n-NA2, -O-(CH2)n-NH2, -O-(CH2)n-NHA,-O-(CH2)n- NA2, -O-(CH2)m-O- vagy R5 csoporttal vannak mono-, di- vagytriszubsztituálva, A jelentése 1-6 szénatomos alkilcsoport, Xhiányzik, vagy jelentése 1-4 szénatomos alkiléncsoport vagykarbonilcsoport, Y hiányzik, vagy jelentése N, HO vagy S, Haljelentése F, Cl, Br vagy I, m értéke 0, 1 vagy 2 és n értéke 0, 1, 2vagy 3 - és sóik Xa alvadási faktor inhibitor hatással rendelkeznek,ezért tromboembóliás betegségek megelőzésére és/vagy kezelésérealkalmazhatók. A találmány tárgya továbbá az (I) általános képletűvegyületeket tartalmazó gyógyszerkészítményekre és a vegyületekelőállítási eljárására is kiterjed. ÓThe new compounds of general formula (I) - in the formula R and R1 are independently H, A, -(CH2)m-R4, -(CH2)m- OA or -(CH2)m-Ar, R2 is Ar, (a ) or (b) a group of general formula, R3 is Ar, R4 is CN, COOH, COOA, CONH2, CONHA, CONA2, or C(=NH)-NH2, R5 is -C(=NH)-NH2, -NH-C (=NH)-NH2 or -C(=O)-N= C(NH2)2, which are unsubstituted or monosubstituted with a -COA, -COOA, -OH group or a conventional amino protecting group, or of formula (c) or (d) group, R6 is H, A or NH2, Ar is fen, naphthyl or biphenyl, which are unsubstituted, or A, 3-6C cycloalkyl, OH, OA, Hal, CN, NO2, CF3, NH2, NHA, NA2, pyrrolidin-1-yl-, piperidin-1-yl-, benzyloxy-, SO2NH2, SO2NHA, SO2NA2,-(CH2)n-NH2, -(CH2)n -NHA, -(CH2)n-NA2, -O- (CH2)n-NH2, -O-(CH2)n-NHA, -O-(CH2)n- NA2, -O-(CH2)m-O- or R5 are mono-, di- or trisubstituted, A means 1- 6-carbon alkyl, X is absent or C1-4 alkylene or carbonyl, Y is absent or N, HO or S, Hal is F, Cl, Br or I, m is 0, 1 or 2 and n is 0, 1, 2 or 3 - and their salts have a coagulation factor Xa inhibitory effect, so they can be used for the prevention and/or treatment of thromboembolic diseases. The subject of the invention also covers pharmaceutical preparations containing compounds of general formula (I) and the process for producing the compounds. HE
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19839499A DE19839499A1 (en) | 1998-08-29 | 1998-08-29 | 2-oxo-2H-quinoline derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0103212A2 true HUP0103212A2 (en) | 2002-05-29 |
| HUP0103212A3 HUP0103212A3 (en) | 2002-06-28 |
Family
ID=7879227
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0103212A HUP0103212A3 (en) | 1998-08-29 | 1999-07-26 | 2-oxo-2h-quinoline derivatives, pharmaceutical compositions containing them and processes for their preparation |
Country Status (17)
| Country | Link |
|---|---|
| EP (1) | EP1107954A1 (en) |
| JP (1) | JP2002523494A (en) |
| KR (1) | KR20010072862A (en) |
| CN (1) | CN1315942A (en) |
| AR (1) | AR021782A1 (en) |
| AU (1) | AU5164199A (en) |
| BR (1) | BR9913140A (en) |
| CA (1) | CA2342230A1 (en) |
| DE (1) | DE19839499A1 (en) |
| HK (1) | HK1042478A1 (en) |
| HU (1) | HUP0103212A3 (en) |
| ID (1) | ID27863A (en) |
| NO (1) | NO20010996L (en) |
| PL (1) | PL346045A1 (en) |
| SK (1) | SK2652001A3 (en) |
| WO (1) | WO2000012479A1 (en) |
| ZA (1) | ZA200102565B (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUE025683T2 (en) | 2002-12-03 | 2016-04-28 | Pharmacyclics Llc | 2-(2-hydroxybiphenyl-3-yl)-1h-benzoimidazole-5-carboxamidine derivatives as factor viia inhibitors |
| CN106573915B (en) | 2014-08-01 | 2020-12-25 | 纽韦卢森公司 | Compounds active against bromodomains |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FI59246C (en) * | 1974-06-24 | 1981-07-10 | Otsuka Pharma Co Ltd | FOERFARANDE FOER FRAMSTAELLNING AV BENSCYKLOAMIDDERIVAT ANVAENDBARA VID TROMBOS- OCH EMBOLITERAPIN |
| IE43079B1 (en) * | 1975-03-20 | 1980-12-17 | Ici Ltd | Quinolone derivatives |
| JPS596858B2 (en) * | 1975-04-30 | 1984-02-15 | オオツカセイヤク カブシキガイシヤ | Method for producing 3,4-dihydrocarbostyryl derivative |
| AT347956B (en) * | 1976-03-18 | 1979-01-25 | Ici Ltd | Process for the preparation of new quinol-2-on-4-yl-alkanoic acids and their base addition salts |
| DE2651581A1 (en) * | 1976-11-12 | 1978-05-18 | Merck Patent Gmbh | CHINOLONE DERIVATIVES AND METHOD FOR THE PRODUCTION THEREOF |
| AU8448491A (en) * | 1990-09-07 | 1992-03-30 | Schering Corporation | Antiviral compounds and antihypertensive compounds |
| DE69128481T2 (en) * | 1990-09-07 | 1998-04-09 | Schering Corp | ANTIVIRAL AND ANTI-HYPERTENSIVE CONNECTIONS |
| ZA928276B (en) * | 1991-10-31 | 1993-05-06 | Daiichi Seiyaku Co | Aromatic amidine derivates and salts thereof. |
| DE4208304A1 (en) * | 1992-03-16 | 1993-09-23 | Merck Patent Gmbh | 2-OXOCHINOLINDERIVATE |
| IL115420A0 (en) * | 1994-09-26 | 1995-12-31 | Zeneca Ltd | Aminoheterocyclic derivatives |
| US5612353A (en) * | 1995-06-07 | 1997-03-18 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Substituted (sulfinic acid, sulfonic acid, sulfonylamino or sulfinylamino) N-[(aminoiminomethyl)phenylalkyl]-azaheterocyclylamide compounds |
| DE19528418A1 (en) * | 1995-08-02 | 1997-02-06 | Merck Patent Gmbh | Endothelin receptor antagonists |
| DE19530996A1 (en) * | 1995-08-23 | 1997-02-27 | Boehringer Mannheim Gmbh | Cyclic guanidines, process for their preparation and pharmaceuticals |
| US5968959A (en) * | 1997-12-12 | 1999-10-19 | Orion Corporation | Method for the prevention and treatment of stunned myocardium |
-
1998
- 1998-08-29 DE DE19839499A patent/DE19839499A1/en not_active Withdrawn
-
1999
- 1999-07-26 KR KR1020017002261A patent/KR20010072862A/en not_active Application Discontinuation
- 1999-07-26 WO PCT/EP1999/005315 patent/WO2000012479A1/en not_active Application Discontinuation
- 1999-07-26 JP JP2000567512A patent/JP2002523494A/en active Pending
- 1999-07-26 BR BR9913140-4A patent/BR9913140A/en not_active Application Discontinuation
- 1999-07-26 PL PL99346045A patent/PL346045A1/en unknown
- 1999-07-26 HU HU0103212A patent/HUP0103212A3/en unknown
- 1999-07-26 EP EP99936606A patent/EP1107954A1/en not_active Withdrawn
- 1999-07-26 AU AU51641/99A patent/AU5164199A/en not_active Abandoned
- 1999-07-26 CA CA002342230A patent/CA2342230A1/en not_active Abandoned
- 1999-07-26 ID IDW20010680A patent/ID27863A/en unknown
- 1999-07-26 CN CN99810283A patent/CN1315942A/en active Pending
- 1999-07-26 SK SK265-2001A patent/SK2652001A3/en unknown
- 1999-08-27 AR ARP990104301A patent/AR021782A1/en unknown
-
2001
- 2001-02-27 NO NO20010996A patent/NO20010996L/en not_active Application Discontinuation
- 2001-03-28 ZA ZA200102565A patent/ZA200102565B/en unknown
-
2002
- 2002-03-25 HK HK02102249.3A patent/HK1042478A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2342230A1 (en) | 2000-03-09 |
| SK2652001A3 (en) | 2001-09-11 |
| WO2000012479A1 (en) | 2000-03-09 |
| ID27863A (en) | 2001-04-26 |
| JP2002523494A (en) | 2002-07-30 |
| HK1042478A1 (en) | 2002-08-16 |
| HUP0103212A3 (en) | 2002-06-28 |
| BR9913140A (en) | 2001-05-08 |
| AR021782A1 (en) | 2002-08-07 |
| NO20010996D0 (en) | 2001-02-27 |
| EP1107954A1 (en) | 2001-06-20 |
| KR20010072862A (en) | 2001-07-31 |
| CN1315942A (en) | 2001-10-03 |
| DE19839499A1 (en) | 2000-03-02 |
| NO20010996L (en) | 2001-02-27 |
| AU5164199A (en) | 2000-03-21 |
| PL346045A1 (en) | 2002-01-14 |
| ZA200102565B (en) | 2002-06-28 |
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